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    Quinazoline derivatives and pharmaceutical compositions containing them
    8.
    再颁专利
    Quinazoline derivatives and pharmaceutical compositions containing them 失效
    喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：USRE42353E1

    公开(公告)日：2011-05-10

    申请号：US12170027

    申请日：1997-09-23

    申请人： Andrew Peter Thomas ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    IPC分类号： C07D239/72 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

    CPC分类号： C07D401/12 ,  A61F13/02 ,  A61F13/023 ,  A61F2013/00221 ,  A61F2013/8408 ,  A61K31/517 ,  A61K31/541 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    摘要翻译： 本发明涉及式（1）的喹唑啉衍生物，其中m为1至2的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或-NR 5 R 6（其中R 5和R 6可以相同或不同，各自表示氢或C 1-3烷基 ）; R2代表氢，羟基，卤代，甲氧基，氨基或硝基; R3表示羟基，卤代，C1-3烷基，C1-3烷氧基，C1-3烷酰氧基，三氟甲基，氰基，氨基或硝基; X 1表示-O - ， - CH 2 - ， - S - ， - SO - ， - SO 2 - ， - NR 7 CO-，-CONR 8 - ， - SO 2 NR 9 - ， - NR 10 SO 2 - 或-NR 11 - （其中R 7，R 8，R 9，R 10 和R 11各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基）; R 4表示任选取代的5或6元饱和碳环或杂环基团或为烯基，炔基或任选取代的烷基的基团，该烷基可含有杂原子连接基团，该烯基，炔基或烷基可带有末端任选取代的 选自烷基和5或6元饱和碳环或杂环基团的基团，及其盐; 其制备方法，含有式（I）化合物或其药学上可接受的盐作为活性成分的药物组合物。 式（I）化合物及其药学上可接受的盐抑制VEGF在治疗许多疾病状态（包括癌症和类风湿性关节炎）中具有价值的性质。

    Chemical compounds
    9.
    发明申请
    Chemical compounds 审中-公开
    化合物

    公开(公告)号：US20090018157A1

    公开(公告)日：2009-01-15

    申请号：US10579552

    申请日：2004-11-25

    申请人： Craig Johnstone ,  Darren McKerrecher ,  Kurt Gordon Pike

    发明人： Craig Johnstone ,  Darren McKerrecher ,  Kurt Gordon Pike

    IPC分类号： A61K31/443 ,  A61P3/04 ,  A61P3/10 ,  C07D405/12 ,  A61K31/4433

    CPC分类号： C07D405/12

    摘要： Compounds of Formula (I) wherein: R1—X— is selected from: methyl, methoxymethyl and Formula (X); R2 is selected from hydrogen, methyl, chloro and fluoro; n is 1 or 2; or a salt, pro-drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

    摘要翻译： 式（I）的化合物，其中：R 1 -X-选自：甲基，甲氧基甲基和式（X）; R2选自氢，甲基，氯和氟; n为1或2; 或其盐，前药或溶剂化物。 还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。

    Benzoyl Amino Pyridyl Carboxylic Acid Derivatives Useful as Glucokinase (Glk) Activators
    10.
    发明申请
    Benzoyl Amino Pyridyl Carboxylic Acid Derivatives Useful as Glucokinase (Glk) Activators 审中-公开
    可用作葡萄糖激酶（Glk）激活剂的苯甲酰基氨基吡啶羧酸衍生物

    公开(公告)号：US20070255062A1

    公开(公告)日：2007-11-01

    申请号：US10579337

    申请日：2004-11-25

    申请人： Craig Johnstone ,  Darren Mckerrecher ,  Kurt Pike

    发明人： Craig Johnstone ,  Darren Mckerrecher ,  Kurt Pike

    IPC分类号： A61K31/44 ,  A61P3/10 ,  C07D211/72

    CPC分类号： C07D213/80

    摘要： Compounds of Formula: (I); wherein: R1 is selected from: fluoro, chloro, C1-3alkyl and C1-3alkoxy; R2—X— is selected from: methyl, methoxymethyl and Formula: (X); n is 0,1 or 2; or a salt, pro-drug or solvate thereof are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.

    摘要翻译： 式（I）化合物： 其中：R 1选自：氟，氯，C 1-3烷基和C 1-3烷氧基; R 2 -X-选自：甲基，甲氧基甲基和式：（X）; n为0,1或2; 或其盐，前药或溶剂化物。 还描述了它们用作GLK活化剂，含有它们的药物组合物及其制备方法。